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    InvivoChem Cat #: V1420
    CAS #: 1373422-53-7Purity ≥98%

    Description: GSKJ1 (GSK-J1; GSK-J 1; GSK-J-1) is a novel, highly selective and potent inhibitor of histone demethylase (H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A) with potential antineoplastic activity. It that has significant activity (IC50 60 nM for human JmjD3) in vitro and in cell assays using an ester prodrug derivative (GSK-J4: 1 µM < IC50 < 10 µM; e.g. 9 µM in primary human macrophages). The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases remove methyl groups from tri- and dimethylated lysine 4 of histone H3. Accumulating evidence from primary tumors and model systems supports a role for KDM5A (JARID1A/RBP2) and KDM5B (JARID1B/PLU1) as oncogenic drivers. The pyridine regio-isomer GSK-J2 displays significantly less on-target activity (IC50 > 100 µM for human JmjD3) and thus can be used as control for target effects in vitro, and as ester derivative (GSK-J5) in cells. Recent data has shown that GSK-J1 also shows some activity (IC50 950 nM for Jarid1b, IC50 1.76 uM for Jarid1c) against H3K4me3/2/1 demethylases.  

    References: Nature. 2012 Aug 16;488(7411):404-8; J Cell Biochem. 2015 Nov;116(11):2628-36

    Related CAS#:1394854-52-4 (GSK-J2); 1797983-09-5 (GSK J4 HCl, prodrug of GSK J1); 1373423-53-0(GSK J4, prodrug of GSK J1); 1797832-71-3 (GSKJ1 sodium)   

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    Molecular Weight (MW)389.45
    CAS No.1373422-53-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 77 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL  
    Synonyms GSKJ1; GSKJ 1; GSKJ-1

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    In Vitro

    In vitro activity: In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3.

    Kinase Assay: purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.

    Cell Assay: Interestingly, the relative selectivity of JIB-04 toward KDM5B over KDM5C in vitro translates to a ~10-50-fold greater growth-inhibitory activity against breast cancer cell lines. 

    In Vivo GSK J4 showed significant growth-inhibitory activity against SF8628 subcutaneous tumors.
    Animal model Mice harboring subcutaneous SF8628 K27M xenografts
    Formulation & Dosage 100 mg/kg/day; i.p.; for 10 days
    ReferencesNature. 2012 Aug 16;488(7411):404-8; J Cell Biochem. 2015 Nov;116(11):2628-36

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Inhibition of GSK-J1 and JIB-04.   2016 Feb 5;291(6):2631-46.


    Structural comparison of KDM5A and KDM6 family demethylases.  2016 Feb 5;291(6):2631-46.


    Overview of demethylation reactions catalyzed by KDM5 family.   2016 Feb 5;291(6):2631-46.


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